Design and synthesis of chlorinated and fluorinated 7-azaindenoisoquinolines as potent cytotoxic anticancer agents that inhibit topoisomerase I

MSA Elsayed, Y Su, P Wang, T Sethi… - Journal of medicinal …, 2017 - ACS Publications
… (1) and the 7-azaindenoisoquinolines produce significantly more DNA damage in an acute
… provides new halogenated 7-azaindenoisoquinolines that are selectively cytotoxic to cancer …

Design and synthesis of indenoisoquinolines targeting topoisomerase I and other biological macromolecules for cancer chemotherapy

M Cushman - Journal of Medicinal Chemistry, 2021 - ACS Publications
… that some of the 7-azaindenoisoquinolines had the ability to … research led to very potent
cytotoxic anticancer agents, it also … rewarded with the extremely cytotoxic 3-fluoro derivative 62 (…

Development in the Synthesis, Topoisomerase I inhibitor and Cytototoxic Properties of Indenoisoquinoline and Its Analogs

D Zeleke, AM Yadessa - Ethiopian Journal of Science and …, 2021 - 213.55.101.19
… chance to develop more effective anticancer drugs in addition to those … Design and Synthesis
of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer

Discovery of 4-alkoxy-2-aryl-6, 7-dimethoxyquinolines as a new class of topoisomerase I inhibitors endowed with potent in vitro anticancer activity

MM Elbadawi, WM Eldehna, W Wang… - European journal of …, 2021 - Elsevier
… potential anticancer agents targeting Topoisomerase I (TOP1), … synthesis of compounds with
different scaffolds can inhibit … TOP1 poisoning activity of the most potent cytotoxic 4-alkoxy-2-…

A comprehensive review of topoisomerase inhibitors as anticancer agents in the past decade

X Liang, Q Wu, S Luan, Z Yin, C He, L Yin, Y Zou… - European journal of …, 2019 - Elsevier
topoisomerase inhibition as antitumor agent in clinical usage. … 2) exhibited the most potent
cytotoxicity against several cell … more potent than camptothecin, and about 6–fold more potent

… of the Pharmacokinetics and Anticancer Activities of Indenoisoquinoline Derivatives That Stabilize the G-Quadruplex in the MYC Promoter and Inhibit Topoisomerase …

Y Han, A Buric, V Chintareddy, M DeMoss… - Journal of Medicinal …, 2024 - ACS Publications
anticancer drugs, dual-downregulation of MYC and … in Raji vs CA-46 cells and cytotoxicity
in MYC-dependent cell lines. … the design and synthesis of new 7-azaindenoisoquinolines and …

2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights

MM Elbadawi, WM Eldehna… - … of Enzyme Inhibition …, 2022 - Taylor & Francis
… Recently, we have developed a new series of 6,7-dimethoxy-4-alkoxy-2-arylquinolines as
Topoisomerase I (TOP1) inhibitors with potent anticancer activity. Utilising the SAR outputs …

Dual DNA topoisomerase 1 and tyrosyl‐DNA phosphodiesterase 1 inhibition for improved anticancer activity

A Zakharenko, N Dyrkheeva… - Medicinal Research …, 2019 - Wiley Online Library
… in 7-azaindenoisoquinolines was also replaced by a chlorine … -chloro and 3-fluoro 7-azaindenoisoquinolines
were less toxic … develop anticancer drugs as both Tdp1 and Tdp2 inhibition

Multiple Topoisomerase I (TopoI), Topoisomerase II (TopoII) and Tyrosyl-DNA Phosphodiesterase (TDP) inhibitors in the development of anticancer drugs

E Baglini, S Salerno, E Barresi, M Robello… - European Journal of …, 2021 - Elsevier
… to inhibition of one class of topoisomerase enzymes is … in the development of potent, efficient
and safe anticancer agents. … only few differences in their cytotoxicity activity, which could …

Indenoisoquinoline Topoisomerase Inhibitors Strongly Bind and Stabilize the MYC Promoter G-Quadruplex and Downregulate MYC

KB Wang, MSA Elsayed, G Wu, N Deng… - Journal of the …, 2019 - ACS Publications
… may hinder intercalation in dsDNA due to possible steric collision with the DNA backbone.
Interestingly, the 3-fluoro-substituted 7-azaindenoisoquinolines 5 … useful anticancer drugs and …